US8324262B2 - Tricyclic necrostatin compounds - Google Patents

Tricyclic necrostatin compounds Download PDF

Info

Publication number
US8324262B2
US8324262B2 US12/086,792 US8679206A US8324262B2 US 8324262 B2 US8324262 B2 US 8324262B2 US 8679206 A US8679206 A US 8679206A US 8324262 B2 US8324262 B2 US 8324262B2
Authority
US
United States
Prior art keywords
carbon atoms
nec
alkyl
och
group
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active, expires
Application number
US12/086,792
Other languages
English (en)
Other versions
US20100190836A1 (en
Inventor
Junying Yuan
Alexei Degterev
Junichi Hitomi
Gregory D. Cuny
Prakash Jagtap
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Harvard College
Brigham and Womens Hospital Inc
Original Assignee
Harvard College
Brigham and Womens Hospital Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Harvard College, Brigham and Womens Hospital Inc filed Critical Harvard College
Priority to US12/086,792 priority Critical patent/US8324262B2/en
Assigned to THE BRIGHAM AND WOMEN'S HOSPITAL, INC. reassignment THE BRIGHAM AND WOMEN'S HOSPITAL, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: CUNY, GREGORY D., JAGTAP, PRAKASH
Assigned to PRESIDENT AND FELLOWS OF HARVARD COLLEGE reassignment PRESIDENT AND FELLOWS OF HARVARD COLLEGE ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: YUAN, JUNYING, DEGTEREV, ALEXEI, HITOMI, JUNICHI
Assigned to NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT reassignment NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT CONFIRMATORY LICENSE (SEE DOCUMENT FOR DETAILS). Assignors: HARVARD UNIVERSITY
Assigned to THE BRIGHAM AND WOMEN'S HOSPITAL, INC. reassignment THE BRIGHAM AND WOMEN'S HOSPITAL, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: CUNY, GREGORY D., JAGTAP, PRAKASH
Assigned to PRESIDENT AND FELLOWS OF HARVARD COLLEGE reassignment PRESIDENT AND FELLOWS OF HARVARD COLLEGE ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: YUAN, JUNYING, DEGTEREV, ALEXEI, HITOMI, JUNICHI
Publication of US20100190836A1 publication Critical patent/US20100190836A1/en
Application granted granted Critical
Publication of US8324262B2 publication Critical patent/US8324262B2/en
Active legal-status Critical Current
Adjusted expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Pyrane Compounds (AREA)
US12/086,792 2005-12-20 2006-12-20 Tricyclic necrostatin compounds Active 2028-10-21 US8324262B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US12/086,792 US8324262B2 (en) 2005-12-20 2006-12-20 Tricyclic necrostatin compounds

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US75191305P 2005-12-20 2005-12-20
US84330406P 2006-09-08 2006-09-08
PCT/US2006/048583 WO2007075772A2 (en) 2005-12-20 2006-12-20 Compounds, screens, and methods of treatment
US12/086,792 US8324262B2 (en) 2005-12-20 2006-12-20 Tricyclic necrostatin compounds

Publications (2)

Publication Number Publication Date
US20100190836A1 US20100190836A1 (en) 2010-07-29
US8324262B2 true US8324262B2 (en) 2012-12-04

Family

ID=38218558

Family Applications (2)

Application Number Title Priority Date Filing Date
US12/086,792 Active 2028-10-21 US8324262B2 (en) 2005-12-20 2006-12-20 Tricyclic necrostatin compounds
US13/665,263 Abandoned US20130158024A1 (en) 2005-12-20 2012-10-31 Tricyclic necrostatin compounds

Family Applications After (1)

Application Number Title Priority Date Filing Date
US13/665,263 Abandoned US20130158024A1 (en) 2005-12-20 2012-10-31 Tricyclic necrostatin compounds

Country Status (7)

Country Link
US (2) US8324262B2 (de)
EP (1) EP1968583A4 (de)
JP (1) JP2009521454A (de)
CN (1) CN101674826A (de)
AU (1) AU2006331754B9 (de)
CA (1) CA2633500A1 (de)
WO (1) WO2007075772A2 (de)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8658689B2 (en) 2007-08-15 2014-02-25 President And Fellows Of Harvard College Heterocyclic inhibitors of necroptosis
US9499521B2 (en) 2014-12-11 2016-11-22 President And Fellows Of Harvard College Inhibitors of cellular necrosis and related methods
US9586880B2 (en) 2008-12-23 2017-03-07 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
US9643977B2 (en) 2011-03-11 2017-05-09 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
US9725452B2 (en) 2013-03-15 2017-08-08 Presidents And Fellows Of Harvard College Substituted indoles and pyrroles as RIP kinase inhibitors
US20180094248A1 (en) * 2016-06-30 2018-04-05 Arizona Board Of Regents On Behalf Of Arizona State University Necroptosis Signaling as a Therapeutic Target for Alzheimer's Disease
US9974774B2 (en) 2013-07-26 2018-05-22 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US10799552B2 (en) * 2011-10-21 2020-10-13 Massachusetts Eye And Ear Infirmary Methods for treating diabetic neurotherapy
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2384753T3 (pl) 2003-08-29 2016-09-30 Pochodne hydantoiny jako inhibitory martwicy komórkowej
CN101353351A (zh) * 2007-07-25 2009-01-28 杨更亮 新的2,3,3a,4-四氢硫色烯并[4,3-c]吡唑类抗炎、抗真菌化合物
BRPI0902039B8 (pt) * 2009-06-09 2021-05-25 Anhanguera Educacional Ltda composição farmacêutica e uso de composição farmacêutica para o tratamento, profilaxia ou prevenção de doenças neoplásicas em humanos e animais
US9073940B2 (en) 2009-11-13 2015-07-07 Merck Serono Sa Tricyclic pyrazol amine derivatives
CN102086212B (zh) * 2009-12-03 2013-06-12 沈阳药科大学 抗真菌剂-2，3，4，5-四氢-4H-苯并[b]噻喃并[4，3-c]吡唑-2-甲酰胺衍生物
WO2011133964A2 (en) 2010-04-23 2011-10-27 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells
WO2012061045A2 (en) 2010-11-01 2012-05-10 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving retinal ganglion cells
WO2013013826A1 (en) * 2011-07-27 2013-01-31 Friedrich-Alexander-Universität Erlangen-Nürnberg Necroptosis inhibitors for the treatment of inflammatory diseases of the gastrointestinal tract
TWI648273B (zh) * 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類（三）
CL2013003785A1 (es) * 2013-12-30 2014-07-11 Univ Pontificia Catolica Chile Uso de necrostatina-1 para el tratamiento de la degeneracion axonal inducida por daños agudos y cronicos
CA2958645A1 (en) * 2014-08-21 2016-02-25 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors as medicaments
WO2016101887A1 (en) * 2014-12-24 2016-06-30 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
CN105078975A (zh) * 2015-07-22 2015-11-25 南方医科大学 Necrostatin-1作为中性粒细胞凋亡促进剂的应用
EP3416725A1 (de) 2016-02-19 2018-12-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Verfahren und pharmazeutische zusammensetzungen zur behandlung von fettleibigkeit
EP3454850B1 (de) * 2016-05-11 2023-06-21 Cumberland Pharmaceuticals Inc. Zusammensetzungen und verfahren zur behandlung von muskeldystrophie mit thromboxan-a2-rezeptor-antagonisten
CN106619619A (zh) * 2017-01-06 2017-05-10 浙江大学 化合物hubin‑1在制备肝脏炎症性疾病预防和/或治疗药物中的用途
CA3052767A1 (en) 2017-02-27 2018-08-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
BR112019020967A2 (pt) * 2017-04-05 2020-05-05 Revolution Medicines Inc métodos e reagentes para analisar interfaces de proteína-proteína
WO2020044206A1 (en) 2018-08-29 2020-03-05 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors for use in the treatment cancer
CN108997183B (zh) * 2018-09-03 2020-02-07 深圳大学 一种二氟甲基化试剂及其制备方法与应用
CN111978311A (zh) * 2019-05-21 2020-11-24 中国科学院上海有机化学研究所 一类细胞程序性坏死抑制剂及其制备方法和用途
CN112263576A (zh) * 2020-09-30 2021-01-26 浙江大学 化合物zju-37在制备肝脏疾病预防和/或治疗药物中的应用
WO2024039250A1 (en) * 2022-08-19 2024-02-22 Pastoral Greenhouse Gas Research Limited Methanogen inhibitors
CN115227692A (zh) * 2022-09-05 2022-10-25 中国医学科学院基础医学研究所 Reblastatin在制备治疗慢性惊厥的药物中的用途

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001028493A2 (en) 1999-10-15 2001-04-26 President And Fellows Of Harvard College Small molecule inhibitors of necrosis
EP1270567A1 (de) 2000-03-21 2003-01-02 Mitsui Chemicals, Inc. Pyrazolinderivate oder tetrahydropyrazolinderivate und deren medizinische verwendung
US6706766B2 (en) 1999-12-13 2004-03-16 President And Fellows Of Harvard College Small molecules used to increase cell death
US6756394B1 (en) * 1999-10-15 2004-06-29 President And Fellow Of Harvard College Small molecule inhibitors of necrosis
US6887993B1 (en) 2003-11-12 2005-05-03 Kosan Biosciences, Inc. 11-O-methylgeldanamycin compounds
WO2006086358A2 (en) 2005-02-10 2006-08-17 Merck & Co., Inc. Mitotic kinesin inhibitors
US7491743B2 (en) 2003-08-29 2009-02-17 President And Fellows Of Harvard College Inhibitors of cellular necrosis
US20100087453A1 (en) 2006-10-10 2010-04-08 President And Fellows Of Harvard College Compounds, screens, and methods of treatment
US20100317701A1 (en) 2007-08-15 2010-12-16 Cuny Gregory D Heterocyclic inhibitors of necroptosis

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002030888A2 (en) * 2000-10-10 2002-04-18 Calyx Therapeutics, Inc. Tricyclic compounds and uses thereof
HRP20020305A8 (en) * 2002-04-10 2009-03-31 GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. 2-thia-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof
JP2004161662A (ja) * 2002-11-13 2004-06-10 Abbott Japan Co Ltd １ｈ−イミダゾキノリン誘導体

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6756394B1 (en) * 1999-10-15 2004-06-29 President And Fellow Of Harvard College Small molecule inhibitors of necrosis
US7253201B2 (en) 1999-10-15 2007-08-07 President And Fellows Of Harvard College Small molecule inhibitors of necrosis
WO2001028493A2 (en) 1999-10-15 2001-04-26 President And Fellows Of Harvard College Small molecule inhibitors of necrosis
US7144905B2 (en) 1999-12-13 2006-12-05 President And Fellows Of Harvard College Small molecules used to increase cell death
US6706766B2 (en) 1999-12-13 2004-03-16 President And Fellows Of Harvard College Small molecules used to increase cell death
US7390836B2 (en) 1999-12-13 2008-06-24 President And Fellows Of Harvard College Small molecules used to increase cell death
EP1270567A1 (de) 2000-03-21 2003-01-02 Mitsui Chemicals, Inc. Pyrazolinderivate oder tetrahydropyrazolinderivate und deren medizinische verwendung
US7491743B2 (en) 2003-08-29 2009-02-17 President And Fellows Of Harvard College Inhibitors of cellular necrosis
US20110144169A1 (en) 2003-08-29 2011-06-16 Cuny Gregory D Inhibitors of cellular necrosis
US6887993B1 (en) 2003-11-12 2005-05-03 Kosan Biosciences, Inc. 11-O-methylgeldanamycin compounds
WO2006086358A2 (en) 2005-02-10 2006-08-17 Merck & Co., Inc. Mitotic kinesin inhibitors
US20100087453A1 (en) 2006-10-10 2010-04-08 President And Fellows Of Harvard College Compounds, screens, and methods of treatment
US20100317701A1 (en) 2007-08-15 2010-12-16 Cuny Gregory D Heterocyclic inhibitors of necroptosis

Non-Patent Citations (22)

* Cited by examiner, † Cited by third party
Title
Australian Patent Office Communication dated Sep. 5, 2011, in Australian Patent Application No. 2006331754.
Chinese Patent Office Action (Application No. 200680053077) dated Feb. 1, 2011.
Chinese Patent Office Communication, dated Nov. 14, 2011, in Chinese Patent Application No. 200680053077.9.
European Patent Office Communication (European Application No. 06847822.1) dated May 5, 2011.
European Search Report (PCT/US2006/048583) dated Aug. 16, 2010.
Fateen et al., "Synthesis of Delta2-Pyrazolines and 1-Naphthols," Egypt J. Chem. 15(4) 329-336 (1972).
Fateen et al., "Synthesis of Δ2-Pyrazolines and 1-Naphthols," Egypt J. Chem. 15(4) 329-336 (1972).
Hammam et al., "Synthesis of Novel Tricyclic Heterocyclic Compounds as Potential Anticancer Agents Using Chromanone and Thiochromanone as Synthons," Indian Journal of Chemistry. 42B: 1985-1993 (2003).
International Preliminary Report on Patentability (PCT/US06/048583), dated Jan. 13, 2009.
International Search Report (PCT/US06/048583), dated Dec. 8, 2008.
Japanese Patent Office Communication dated Aug. 20, 2012, in Japanese Patent Application No. 2008-547482.
Office Action pertaining to U.S. Appl. No. 09/688,015, mailed Mar. 7, 2002.
Office Action pertaining to U.S. Appl. No. 09/688,015, mailed May 30, 2001.
Office Action pertaining to U.S. Appl. No. 09/688,015, mailed Nov. 5, 2002.
Office Action pertaining to U.S. Appl. No. 10/880,377, mailed Jul. 20, 2006.
Office Action pertaining to U.S. Appl. No. 10/880,377, mailed Mar. 17, 2006.
Peesapati et al., "Nitrogen Heterocyclic Systems: Synthesis of 3,3a-trans and cis-2-acetyl/phenyl-3-arylhexahydobenzo[6,7] cyclohepta[1,2-c]pyrazoles," J. Chem. Research. S: 372-374 (2001).
Sangwan, "Use of Characteristic 1H N.M.R. Chemical Shifts to Differentiate Diastereoisomeric [1]Benzopyrano-[4,3-c]pyrazoles, Pyrazolo[4,3-c]quinlines, and Related Compounds," J. Chem. Research. 5: 22-23 (1987).
Sinha et al., "Synthesis of 3, 3a-trans/cis-2-Phenyl/Acetyl-3-Aryl-Tetrahydroindeno/napntho [1, 2-c]- and Hexahydrobenzo [6,7]cyclophepta[1,2-c]pyrazoles as Antiimplantation Agents," Indian Journal of Chemistry. 30B: 684-692 (1991).
Teng et al.,"Structure-Activity Relationship Study of Novel Necroptosis Inhibitors," Bioorg Med Chem Lett. 15:5039-5044 (2005).
U.S. Appl. No. 13/141,545, filed Jun. 22, 2011, Yuan et al.
Written Opinion of the International Search Authority (PCT/US06/048583), dated Nov. 21, 2008.

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8658689B2 (en) 2007-08-15 2014-02-25 President And Fellows Of Harvard College Heterocyclic inhibitors of necroptosis
US9108955B2 (en) 2007-08-15 2015-08-18 President And Fellows Of Harvard College Heterocyclic inhibitors of necroptosis
US9586880B2 (en) 2008-12-23 2017-03-07 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
US9643977B2 (en) 2011-03-11 2017-05-09 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
US10799552B2 (en) * 2011-10-21 2020-10-13 Massachusetts Eye And Ear Infirmary Methods for treating diabetic neurotherapy
US9725452B2 (en) 2013-03-15 2017-08-08 Presidents And Fellows Of Harvard College Substituted indoles and pyrroles as RIP kinase inhibitors
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
US9974774B2 (en) 2013-07-26 2018-05-22 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US9993460B2 (en) 2013-07-26 2018-06-12 Race Oncology Ltd. Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US10500192B2 (en) 2013-07-26 2019-12-10 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US10548876B2 (en) 2013-07-26 2020-02-04 Race Oncology Ltd. Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US11135201B2 (en) 2013-07-26 2021-10-05 Race Oncology Ltd. Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US11147800B2 (en) 2013-07-26 2021-10-19 Race Oncology Ltd. Combinatorial methods to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
US9944628B2 (en) 2014-12-11 2018-04-17 President And Fellows Of Harvard College Inhibitors of cellular necrosis and related methods
US10508102B2 (en) 2014-12-11 2019-12-17 President And Fellows Of Harvard College Inhibitors of cellular necrosis and related methods
US9499521B2 (en) 2014-12-11 2016-11-22 President And Fellows Of Harvard College Inhibitors of cellular necrosis and related methods
US20180094248A1 (en) * 2016-06-30 2018-04-05 Arizona Board Of Regents On Behalf Of Arizona State University Necroptosis Signaling as a Therapeutic Target for Alzheimer's Disease

Also Published As

Publication number Publication date
WO2007075772A3 (en) 2009-02-19
EP1968583A2 (de) 2008-09-17
WO2007075772A2 (en) 2007-07-05
JP2009521454A (ja) 2009-06-04
AU2006331754B9 (en) 2013-07-11
AU2006331754A1 (en) 2007-07-05
AU2006331754A2 (en) 2008-08-14
AU2006331754B2 (en) 2013-07-04
EP1968583A4 (de) 2010-09-15
US20100190836A1 (en) 2010-07-29
CN101674826A (zh) 2010-03-17
CA2633500A1 (en) 2007-07-05
US20130158024A1 (en) 2013-06-20

Similar Documents

Publication Publication Date Title
US8324262B2 (en) Tricyclic necrostatin compounds
CA2666060C (en) Thieno[2,3-d]pyrimidin-4-one compounds and methods of using the same
US9725452B2 (en) Substituted indoles and pyrroles as RIP kinase inhibitors
AU2012208526B2 (en) Fused aminodihydrothiazine derivatives useful as BACE inhibitors
DK2556071T3 (en) Kinase inhibitors AND THEIR USE FOR THE TREATMENT OF CANCER
WO2014152182A1 (en) Deuterated heterocyclic inhibitors of necroptosis
AU2016378108B9 (en) 4-hydroxy-2-phenyl-1,3-thiazol-5-yl methanone derivatives as TRPM8 antagonists
JP2024517861A (ja) ＰＫＣ－θモジュレーター
JP2011515493A (ja) 抗原受容体により誘導されるＮＦ−κＢの活性化の阻害剤
Sakla et al. Development of Benzimidazole-Substituted Spirocyclopropyl Oxindole Derivatives as Cytotoxic Agents: Tubulin Polymerization Inhibition and Apoptosis Inducing Studies

Legal Events

Date Code Title Description
AS Assignment

Owner name: THE BRIGHAM AND WOMEN'S HOSPITAL, INC., MASSACHUSE

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:CUNY, GREGORY D.;JAGTAP, PRAKASH;SIGNING DATES FROM 20070413 TO 20070416;REEL/FRAME:019228/0463

AS Assignment

Owner name: PRESIDENT AND FELLOWS OF HARVARD COLLEGE, MASSACHU

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:YUAN, JUNYING;DEGTEREV, ALEXEI;HITOMI, JUNICHI;SIGNING DATES FROM 20070228 TO 20070822;REEL/FRAME:021579/0626

AS Assignment

Owner name: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF

Free format text: CONFIRMATORY LICENSE;ASSIGNOR:HARVARD UNIVERSITY;REEL/FRAME:022171/0884

Effective date: 20081223

AS Assignment

Owner name: THE BRIGHAM AND WOMEN'S HOSPITAL, INC., MASSACHUSE

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:CUNY, GREGORY D.;JAGTAP, PRAKASH;SIGNING DATES FROM 20070413 TO 20070416;REEL/FRAME:022227/0925

Owner name: PRESIDENT AND FELLOWS OF HARVARD COLLEGE, MASSACHU

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:YUAN, JUNYING;DEGTEREV, ALEXEI;HITOMI, JUNICHI;SIGNING DATES FROM 20070228 TO 20070822;REEL/FRAME:022227/0989

STCF Information on status: patent grant

Free format text: PATENTED CASE

FEPP Fee payment procedure

Free format text: PAT HOLDER NO LONGER CLAIMS SMALL ENTITY STATUS, ENTITY STATUS SET TO UNDISCOUNTED (ORIGINAL EVENT CODE: STOL); ENTITY STATUS OF PATENT OWNER: LARGE ENTITY

FPAY Fee payment

Year of fee payment: 4

MAFP Maintenance fee payment

Free format text: PAYMENT OF MAINTENANCE FEE, 8TH YEAR, LARGE ENTITY (ORIGINAL EVENT CODE: M1552); ENTITY STATUS OF PATENT OWNER: LARGE ENTITY

Year of fee payment: 8

CC Certificate of correction